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CU20110190A7 - ANALOGS OF ISOXAZOL-3 (2H) -ONA AS THERAPEUTIC AGENTS - Google Patents

ANALOGS OF ISOXAZOL-3 (2H) -ONA AS THERAPEUTIC AGENTS

Info

Publication number
CU20110190A7
CU20110190A7 CU20110190A CU20110190A CU20110190A7 CU 20110190 A7 CU20110190 A7 CU 20110190A7 CU 20110190 A CU20110190 A CU 20110190A CU 20110190 A CU20110190 A CU 20110190A CU 20110190 A7 CU20110190 A7 CU 20110190A7
Authority
CU
Cuba
Prior art keywords
alkyl
optionally substituted
aryl
heteroaryl
atoms
Prior art date
Application number
CU20110190A
Other languages
Spanish (es)
Inventor
Peter Schell
Daniel Pettersen
Michael Karle
Tomas Fex
Leifeng Cheng
Jonas Bostroem
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of CU20110190A7 publication Critical patent/CU20110190A7/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Un compuesto de fórmula I ESPACIO PARA LA FÓRMULA o una sal farmacéuticamente aceptable de este, donde R1 y R2 son independientemente hidrógeno, deuterio, arilo, heteroarilo, alquilo C1-C8, y están opcionalmente sustituidos con uno o más sustituyentes que son independientemente R3, R3 es un arilo, heteroarilo, uno o más átomos de flúor, un alquilo C1-C6 que contiene uno o más átomos de flúor, un alquilo C1-C6 que contiene uno o más átomos de deuterio, un alquilo C1-C6 que contiene hidroxi, estando el arilo y el heteroarilo opcionalmente sustituidos con uno o más halógenos, un alcoxi fluorado, un alquilo fluorado, un sulfonilo, uno o más átomos de deuterio, un alquilo C1-C6, un alcoxi C1-C6, un nitrilo, o R3 es un alquilo C1-C6 opcionalmente sustituido con uno o más de los siguientes grupos: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; donde R4 es un alquilo C1-C10 opcionalmente sustituido con uno o más átomos de flúor, deuterio, alcoxi, carboxilato de arilo, carboxilato de alquilo; R5 y R6 se seleccionan independientemente entre hidrógeno, alquilo o pueden formar conjuntamente un anillo de carbono de 4-8 miembros; o R1 y R2 forman un anillo de carbono de 3-10 miembros que comprende opcionalmente O ó N y está opcionalmente sustituido con un alquilo o arilo C1-C10, heteroarilo opcionalmente sustituido con R3.A compound of formula I SPACE FOR THE FORMULA or a pharmaceutically acceptable salt thereof, where R1 and R2 are independently hydrogen, deuterium, aryl, heteroaryl, C1-C8 alkyl, and are optionally substituted with one or more substituents that are independently R3, R3 is an aryl, heteroaryl, one or more fluorine atoms, a C1-C6 alkyl containing one or more fluorine atoms, a C1-C6 alkyl containing one or more deuterium atoms, a C1-C6 alkyl containing hydroxy , the aryl and heteroaryl being optionally substituted with one or more halogens, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium atoms, a C1-C6 alkyl, a C1-C6 alkoxy, a nitrile, or R3 it is a C1-C6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein R4 is a C1-C10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, aryl carboxylate, alkyl carboxylate atoms; R5 and R6 are independently selected from hydrogen, alkyl or can together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring which optionally comprises O or N and is optionally substituted with a C1-C10 alkyl or aryl, heteroaryl optionally substituted with R3.

CU20110190A 2009-04-07 2011-10-07 ANALOGS OF ISOXAZOL-3 (2H) -ONA AS THERAPEUTIC AGENTS CU20110190A7 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16722409P 2009-04-07 2009-04-07
US17195609P 2009-04-23 2009-04-23

Publications (1)

Publication Number Publication Date
CU20110190A7 true CU20110190A7 (en) 2012-02-15

Family

ID=42934883

Family Applications (1)

Application Number Title Priority Date Filing Date
CU20110190A CU20110190A7 (en) 2009-04-07 2011-10-07 ANALOGS OF ISOXAZOL-3 (2H) -ONA AS THERAPEUTIC AGENTS

Country Status (21)

Country Link
US (1) US8415378B2 (en)
EP (1) EP2417131A4 (en)
JP (1) JP5711723B2 (en)
KR (1) KR101675607B1 (en)
CN (1) CN102459246B (en)
AR (1) AR076219A1 (en)
AU (1) AU2010235236B2 (en)
BR (1) BRPI1013984A2 (en)
CA (1) CA2757879C (en)
CO (1) CO6440580A2 (en)
CU (1) CU20110190A7 (en)
EA (1) EA020825B1 (en)
EC (1) ECSP11011385A (en)
IL (1) IL215336A0 (en)
MX (1) MX2011010647A (en)
NI (1) NI201100181A (en)
SG (1) SG174463A1 (en)
TW (1) TW201040166A (en)
UY (1) UY32543A (en)
WO (1) WO2010117323A1 (en)
ZA (1) ZA201108119B (en)

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CN102977050B (en) * 2012-11-20 2015-04-22 浙江工业大学 Method for synthesizing 2-benzothiazolyl dimethylacetal and 2-benzothiazol formaldehyde
CN102977040B (en) * 2012-11-20 2015-06-03 浙江工业大学 Method for synthesizing 2-quinoxalinyl dimethylacetal and 2-quinoxalinyl formaldehyde
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
ES2657451T3 (en) 2013-04-19 2018-03-05 Incyte Holdings Corporation Bicyclic heterocyclics as FGFR inhibitors
UY35809A (en) 2013-11-05 2015-05-29 Bayer Pharma AG (AZA) PIRIDOPIRAZOLOPIRIMIDINONAS AND INDAZOLOPIRIMIDINONAS AND ITS USES
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AU2015363700A1 (en) 2014-12-19 2017-04-27 Emeriti Pharma Ab 3-(piperidin-4-yl)-isoxazol-3(2H)-ones for treatment of dermatologic disorders
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CN107857725A (en) * 2017-12-19 2018-03-30 苏州艾缇克药物化学有限公司 A kind of synthetic method of the methanol of 2 aminopyridine 4
MX2020011639A (en) 2018-05-04 2021-02-15 Incyte Corp Salts of an fgfr inhibitor.
KR20210018265A (en) 2018-05-04 2021-02-17 인사이트 코포레이션 Solid form of FGFR inhibitor and method for preparing same
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Also Published As

Publication number Publication date
AR076219A1 (en) 2011-05-26
JP2012522836A (en) 2012-09-27
KR20120034611A (en) 2012-04-12
EP2417131A1 (en) 2012-02-15
KR101675607B1 (en) 2016-11-11
UY32543A (en) 2010-11-30
TW201040166A (en) 2010-11-16
US8415378B2 (en) 2013-04-09
ECSP11011385A (en) 2011-11-30
BRPI1013984A2 (en) 2018-06-19
CN102459246B (en) 2014-05-07
EA201190237A1 (en) 2012-04-30
AU2010235236B2 (en) 2013-10-24
CN102459246A (en) 2012-05-16
NI201100181A (en) 2012-06-14
CO6440580A2 (en) 2012-05-15
MX2011010647A (en) 2012-02-21
JP5711723B2 (en) 2015-05-07
IL215336A0 (en) 2011-12-29
US20100261755A1 (en) 2010-10-14
SG174463A1 (en) 2011-10-28
WO2010117323A8 (en) 2010-11-18
AU2010235236A1 (en) 2011-10-20
CA2757879A1 (en) 2010-10-14
EP2417131A4 (en) 2014-08-27
EA020825B1 (en) 2015-02-27
CA2757879C (en) 2017-06-06
WO2010117323A1 (en) 2010-10-14
ZA201108119B (en) 2012-07-25

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